Disulfide-linked liposomes: Effective delivery vehicle for Bcl-2 antisense oligodeoxyribonucleotide G3139

Wanlop Weecharangsan, Bo Yu, Shujun Liu, JiuXia Pang, L. James Lee, Guido Marcucci, Robert J. Lee

Research output: Contribution to journalArticlepeer-review

7 Scopus citations


Background: Disulfide-linked oligodeoxyribonucleotide (ODN) liposomes were formulated and evaluated for the delivery of antisense ODN G3139 in KB human oral carcinoma cells. Materials and Methods: Liposomes composed of 1,2-di-(9Z-octadecenoyl)-3-trimethylammo-nium-propane(DOTAP)/egg phosphatidylcholine/α-tocopheryl polyethylene glycol 1000 succinate were incorporated with hydrophobized disulfide-linked ODN. Disulfide-linked ODN liposomes were characterized for their size, ODN intracellular delivery, Bcl-2 mRNA and protein expression, growth inhibition, and chemosensitization. Results: Intracellular delivery of ODN with disulfide-linked ODN liposomes was more efficient than that with non-liposomal hydrophobized disulfide-linked ODN. Treatment of the cells with disulfide-linked ODN liposomes resulted in efficient Bcl-2 down-regulation greater than that with hydrophobized disulfide-linked ODN and consistent with that of cellular growth inhibition and the sensitization to daunorubicin in KB cells. Disulfide-linked ODN liposomes exhibited superior colloidal stability during 5-week storage. Conclusion: Disulfide-linked liposomes are effective delivery vehicles for antisense ODN.

Original languageEnglish (US)
Pages (from-to)31-38
Number of pages8
JournalAnticancer Research
Issue number1
StatePublished - Jan 2010
Externally publishedYes


  • Antisense oligonucleotide
  • Bcl-2
  • Disulfide
  • Drug delivery
  • G3139
  • Liposomes


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